BRPI0409698A - triaza- and tetraaza-anthracenedione derivatives, their preparation and their use as pharmaceuticals - Google Patents

triaza- and tetraaza-anthracenedione derivatives, their preparation and their use as pharmaceuticals

Info

Publication number
BRPI0409698A
BRPI0409698A BRPI0409698-3A BRPI0409698A BRPI0409698A BR PI0409698 A BRPI0409698 A BR PI0409698A BR PI0409698 A BRPI0409698 A BR PI0409698A BR PI0409698 A BRPI0409698 A BR PI0409698A
Authority
BR
Brazil
Prior art keywords
alkyl
phenyl
triaza
tetraaza
pyridinyl
Prior art date
Application number
BRPI0409698-3A
Other languages
Portuguese (pt)
Inventor
Andreas Weichert
Hartmut Strobel
Paulus Wohlfahrt
Marcel Patek
Martin Smrcina
Aleksandra Weichsel
Original Assignee
Sanofi Aventis Deutschland
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Sanofi Aventis Deutschland filed Critical Sanofi Aventis Deutschland
Publication of BRPI0409698A publication Critical patent/BRPI0409698A/en

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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/12Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
    • C07D471/14Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/08Bronchodilators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
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    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/10Drugs for genital or sexual disorders; Contraceptives for impotence
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/02Non-specific cardiovascular stimulants, e.g. drugs for syncope, antihypotensives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/06Antiarrhythmics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/14Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Life Sciences & Earth Sciences (AREA)
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  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Diabetes (AREA)
  • Pulmonology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Vascular Medicine (AREA)
  • Hematology (AREA)
  • Hospice & Palliative Care (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Endocrinology (AREA)
  • Urology & Nephrology (AREA)
  • Obesity (AREA)
  • Emergency Medicine (AREA)
  • Ophthalmology & Optometry (AREA)
  • Psychiatry (AREA)
  • Gynecology & Obstetrics (AREA)
  • Reproductive Health (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

A triaza- and tetraaza-anthracenedione derivatives, its stereoisomeric forms or mixture, or salts are new. A triaza- and tetraaza-anthracenedione derivatives of formula (I), its stereoisomeric forms or mixture, or salts are new. [Image] A : CR 6 or N; B : CR 7 or N; R 11-10C alkyl, 3-8C cycloalkyl, 2-10C alkenyl or 2-10C alkynyl (all optionally substituted by halo, CN, 3-8C cycloalkyl, phenyl, biphenylyl, naphthyl, indanyl or heteroaryl); R 2H, 1-4C alkyl, CF 3, -(CH 2) a-3-8C cycloalkyl, -(CH 2) a-phenyl, -(CH 2) a-imidazolyl or -(CH 2) a-pyridinyl; a : 0 - 2; R 3-(CH 2) b-phenyl, -(CH 2) b-imidazolyl, -(CH-2) b-triazolyl, -(CH 2) b-Het or -(CH 2) b-pyridinyl; b : 1 - 4; R 4 - R 7H, 1-4C alkyl, CF 3, 1-4C alkoxy, OCF 3, halo, nitro, CN, -CO-R 1 0, -NR 8R 9, -NH-CO-1-4C alkyl, -SO 2-NR 8R 9, -SO 2-1-4C alkyl or -SO 2-(CH 2) c-phenyl; c : 0 - 2; R 8 and R 9H or 1-4C alkyl; R 1 0OH, 1-4C alkoxy or -NR 8R 9; Het : a residue of a saturated 5- or 6-membered monocyclic heterocycle (contains a ring nitrogen via which it is bonded, and additionally contains a further ring heteroatom selected from N, O and S, and optionally substituted by 1-4C alkyl or -(CH 2) d-phenyl); d : 0 - 2; Heteroaryl : a residue of an aromatic 5 - 10 membered, monocyclic or bicyclic heterocycle (contains 1 - 4 N, O and S). The residues phenyl, biphenylyl, naphthyl, indanyl, heteroaryl, pyridinyl, imidazolyl and triazolyl are optionally substituted by halo, CN, 1-6C alkyl, CF 3, 1-6C alkoxy or OCF 3. A and B are not simultaneously N. An independent claim is included for preparation of (I). ACTIVITY : Cardiovascular-Gen.; Antianginal; Cardiant; Cerebroprotective; Vasotropic; Thrombolytic; Antiarteriosclerotic; Hypotensive; Respiratory-Gen.; Nephrotropic; Antiarrhythmic; Antidiabetic; Ophthalmological; Antiasthmatic; Antiangiogenic; Hepatotropic; Osteopathic. MECHANISM OF ACTION : Endothelial nitric oxide (NO) synthase (eNOS) expression stimulator. (4S)-9-(3-(Imidazo)-1-yl)propyl)-4-isopropyl-6-nitro-2-(4-phenylbutyl)-1,2,9,9a-tetrahydro-2,4a,9-triaza-anthracene- 3,10(4H)-dione trifluoroacetic acid (Ia) was tested for activation of eNOS transcription as described in Li et al., Activation of protein kinase C alpha and/or epsilon enhances transcription of the human endothelial nitric oxide synthase gene, Mol. Pharmacol. 53 (1998) 630. (Ia) Showed an EC 5 0 of 2.2 mM.
BRPI0409698-3A 2003-04-24 2004-04-13 triaza- and tetraaza-anthracenedione derivatives, their preparation and their use as pharmaceuticals BRPI0409698A (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP20030009286 EP1471066A1 (en) 2003-04-24 2003-04-24 Triaza- and tetraaza-anthracenedione derivates, their preparation and their use as pharmaceuticals
PCT/EP2004/003851 WO2004094425A1 (en) 2003-04-24 2004-04-13 Triaza- and tetraaza-anthracenedione derivatives, their preparation and their use as pharmaceuticals

Publications (1)

Publication Number Publication Date
BRPI0409698A true BRPI0409698A (en) 2006-04-18

Family

ID=32946872

Family Applications (1)

Application Number Title Priority Date Filing Date
BRPI0409698-3A BRPI0409698A (en) 2003-04-24 2004-04-13 triaza- and tetraaza-anthracenedione derivatives, their preparation and their use as pharmaceuticals

Country Status (13)

Country Link
EP (2) EP1471066A1 (en)
JP (1) JP4603530B2 (en)
AT (1) ATE501144T1 (en)
AU (1) AU2004232456B2 (en)
BR (1) BRPI0409698A (en)
CA (1) CA2523196C (en)
DE (1) DE602004031734D1 (en)
DK (1) DK1641795T3 (en)
ES (1) ES2362658T3 (en)
IL (1) IL171500A (en)
MX (1) MXPA05011267A (en)
PT (1) PT1641795E (en)
WO (1) WO2004094425A1 (en)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ATE421518T1 (en) 2005-02-10 2009-02-15 Bristol Myers Squibb Co DIHYDROQUINAZOLINONES AS 5HT MODULATORS
EP1741709A1 (en) 2005-06-28 2007-01-10 Sanofi-Aventis Deutschland GmbH Heteroaryl-substituted amides comprising a saturated linker group, and their use as pharmaceuticals
EP1741708A1 (en) 2005-06-28 2007-01-10 Sanofi-Aventis Deutschland GmbH Heteroaryl-substituted amides comprising an unsaturated or cyclic linker group, and their use as pharmaceuticals
EP1905764A1 (en) 2006-09-30 2008-04-02 Sanofi-Aventis Substituted 2-Phenyl-benzimidazoles and their use as pharmaceuticals
EP1923062A1 (en) 2006-11-16 2008-05-21 sanofi-aventis Imidazo[2,1-b]thiazoles and their use as pharmaceuticals
EP1942104A1 (en) 2006-12-20 2008-07-09 sanofi-aventis Heteroarylcyclopropanecarboxamides and their use as pharmaceuticals
EP1939180A1 (en) 2006-12-20 2008-07-02 sanofi-aventis Heteroarylacrylamides and their use as pharmaceuticals for the stimulation of the expression of endothelial NO synthase
EP1939181A1 (en) 2006-12-27 2008-07-02 sanofi-aventis Heteroaryl-substituted carboxamides and use thereof for the stimulation of the expression of NO synthase
EP1964841A1 (en) 2007-02-28 2008-09-03 sanofi-aventis Imidazo[1,2-a]azine and their use as pharmaceuticals
EP1964840A1 (en) 2007-02-28 2008-09-03 sanofi-aventis Imidazo[1,2-a]pyridines and their use as pharmaceuticals
GB2575490A (en) * 2018-07-12 2020-01-15 Recordati Ind Chimica E Farmaceutica Spa P2X3 receptor antagonists
WO2021048364A1 (en) * 2019-09-11 2021-03-18 Solvay Sa Process for manufacturing a substituted cyclohexanecarbonitrile

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6294517B1 (en) * 1996-02-02 2001-09-25 Nitromed, Inc. Compositions and kits comprising alpha-adrenergic receptor antagonists and nitric oxide donors and methods of use
PE20020856A1 (en) * 2001-02-13 2002-11-11 Aventis Pharma Gmbh 1,2,3,4-TETRAHYDRONAFTIL ACILATED AMINES

Also Published As

Publication number Publication date
AU2004232456B2 (en) 2010-06-17
EP1641795A1 (en) 2006-04-05
DE602004031734D1 (en) 2011-04-21
EP1471066A1 (en) 2004-10-27
WO2004094425A1 (en) 2004-11-04
EP1641795B1 (en) 2011-03-09
JP4603530B2 (en) 2010-12-22
ATE501144T1 (en) 2011-03-15
CA2523196A1 (en) 2004-11-04
MXPA05011267A (en) 2006-05-25
AU2004232456A1 (en) 2004-11-04
JP2006524197A (en) 2006-10-26
ES2362658T3 (en) 2011-07-11
DK1641795T3 (en) 2011-06-27
CA2523196C (en) 2012-05-29
PT1641795E (en) 2011-05-18
IL171500A (en) 2010-06-30

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Legal Events

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B06F Objections, documents and/or translations needed after an examination request according [chapter 6.6 patent gazette]
B08F Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette]

Free format text: REFERENTE A 10A ANUIDADE.

B08K Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette]

Free format text: REFERENTE AO DESPACHO 8.6 PUBLICADO NA RPI 2259 DE 22/04/2014.